咔啉类衍生物与小牛胸腺DNA的结合──结合方式及结合强度的测定

咔啉类衍生物与小牛胸腺DNA的结合──结合方式及结合强度的测定

杨铭, 王夔, 藏传兵, 王保怀, 张有民

1. 北京医科大学天然及仿生药物国家重点实验室, 北京 100083;
2. 北京大学物理化学研究所, 北京 100871

收稿日期:1992-05-09 修回日期:1993-10-08 出版日期:1994-06-15 发布日期:1994-06-15

Binding of Carboline Derivatives to Calf Thymus DNA─Determination of Binding Mode and Binding Strength

Ming Yang, Kui Wang, Chuan-Bing Zang, Bao-Huai Wang, You-MinZhang

1. National Research haboratories of Natural and Biomimetic Drugs, Beijing Medical University, Beijing 100083;
2. Institute of Physical Chemistry, Peking University, Beijing 100871

Received:1992-05-09 Revised:1993-10-08 Online:1994-06-15 Published:1994-06-15

摘要/Abstract

摘要： 研究了六个咔啉类衍生物(CB1-6)与DNA结合的方式, 强度及与其抗肿瘤活性的关系。通过DNA双螺旋结构的变化, 包括粘度、³¹P NMR、CD谱的测定及CB1-6在用DNA滴定过程中, uv-Vis光谱的减色效应和化合物芳环质子的¹H NMR谱的变化来阐明CB1-6与DNA的结合方式; 通过光谱法及微量量热测定了与DNA的结合强度。测定数据表明结合强度与环的芳香性及取代基有很强的依赖性, 此结果在生物测定中得到证实。

关键词: ；大学DNA, 咔啉, 结合方式, 结合强度

Abstract: The relationship between anticancer activity of six carboline derivatives (CB1-6)and their binding mode and binding strength with DNA was studied. Binding mode was established by study of structural changes in DNA helix, which involved assessment of changes in the viscosity, ³¹P NMR and CD spectra of DNA as well as hypochromism in UV-Vis determination and ¹H NMR spectra of the aromatic protons of CB1-6 by titration with DNA. Binding strength was evaluated by spectroscopic and microcalorimetric measurements. The results indicate that the binding depends strongly on the ring automaticity and the substituent groups, which accords well with the findings in bioactivity tests.

Key words: DNA, Carboline, Binding mode, Binding strength

Supporting:

杨铭, 王夔, 藏传兵, 王保怀, 张有民. 咔啉类衍生物与小牛胸腺DNA的结合──结合方式及结合强度的测定[J]. .

Ming Yang, Kui Wang, Chuan-Bing Zang, Bao-Huai Wang, You-MinZhang. Binding of Carboline Derivatives to Calf Thymus DNA─Determination of Binding Mode and Binding Strength[J]. .

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